作为对Trichomonas vaginalis的抗药剂的酸盐
Lígia R Oliveira1, Márcia R Trein2, Letícia R Assis1
1Institute of Biosciences, Humanities and Exact Sciences (Ibilce), São Paulo State University (Unesp), 15054-000 São José do Rio Preto, SP, Brazil.
Bioorganic chemistry
|October 15, 2023
概括
一种新型的类,4-基 (4HC),对Trichomonas vaginalis,即三病的原因,显示出有前途. 这种化合物是这种常见的性传播感染的潜在新疗法.
科学领域:
- 药用化学 医学化学
- 寄生虫学的寄生虫学
- 药物发现 药物发现 药物发现
背景情况:
- 三,一个常见的性传播感染,由Trichomonas vaginalis引起,越来越多地抵抗目前的胺治疗.
- 迫切需要新型治疗药物来对抗耐药性Trichomonas vaginalis感染.
研究的目的:
- 设计,合成和评估新型酸盐作为潜在的抗T. vaginalis剂.
- 确定最强效的化合物,阐明其作用机制和安全性.
主要方法:
- 合成了21种酸,并评估了它们对T. vaginalis trophozoites的活性.
- 在体外和体外毒性评估 (人体红细胞,Galleria mellonella幼虫).
- 对活性氧物种 (ROS) 生成,基因表达 (PFOR,β-tubulin) 和与T. vaginalis纯核酸酸酶 (TvPNP) 在体对接的分析.
主要成果:
- 结构-活性关系研究发现4'-基 (4HC) 是最活跃的化合物 (IC50 = 27.5μM).
- 4HC在体外和体内没有显著的毒性.
- 与T. vaginalis共同化的中性粒细胞中的4HC调节的ROS水平,但没有影响PFOR或β-tubulin基因表达.
- 在分析证实了4HC作为TvPNP的配体的潜力.
结论:
- 酸,特别是4HC,代表了一种有前途的新类化合物,用于开发针对Trichomonas vaginalis的治疗方法.
- 4HC的良好的安全性和特定的作用机制要求对抗三病进行进一步的研究.
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